Enoximone is a selective phosphodiesterase inhibitor with vasodilating and positive inotropic activity that does not cause changes in myocardial oxygen consumption. It is used in patients with congestive heart failure. Trials were halted in the U.S., but the drug is used in various countries.
|External IDs||MDL 17,043 / MDL-17043|
|Product Ingredients||Not Available|
|Approved Prescription Products||Not Available|
|Approved Generic Prescription Products||Not Available|
|Approved Over the Counter Products||Not Available|
|Unapproved/Other Products||Not Available|
|Brand mixtures||Not Available|
|Weight||Average: 248.301 |
For the treatment of congestive heart failure.
|Structured Indications||Not Available|
Enoximone is a phosphodiesterase inhibitor (type III) that increases the force of contraction of the heart and dilates blood vessels. In June 2005, Myogen announced that they were discontinuing development of enoximone due to negative results. The drug is approved for use in the UK.
|Mechanism of action|
Further research is required to determine accurately the mechanism of action of drugs with phosphodiesterase inhibitory activity, however, inhibition of PDE3 inhibits degredation of cGMP. This allows for increased NO release and vascular relaxation.
Bioavailabvility is 50% following oral administration.
|Volume of distribution||Not Available|
|Route of elimination||Not Available|
|Pharmacogenomic Effects/ADRs||Not Available|
|Drug Interactions||Not Available|
|Food Interactions||Not Available|
|Synthesis Reference||Not Available|
|ATC Codes||C01CE03 — Enoximone|
|AHFS Codes||Not Available|
|PDB Entries||Not Available|
|FDA label||Not Available|
|Dosage forms||Not Available|
|Predicted ADMET features|
|Mass Spec (NIST)||Not Available|
|Description||This compound belongs to the class of chemical entities known as aryl-phenylketones. These are aromatic compounds containing a ketone substituted by one aryl group, and a phenyl group.|
|Super Class||Organic compounds|
|Class||Organic oxygen compounds|
|Sub Class||Organooxygen compounds|
|Alternative Parents||Thiophenol ethers / Benzoyl derivatives / Carbonylimidazoles / Alkylarylthioethers / Vinylogous amides / Heteroaromatic compounds / Ureas / Sulfenyl compounds / Azacyclic compounds / Organopnictogen compounds / Organonitrogen compounds / Organic oxides / Hydrocarbon derivatives|
|Substituents||Aryl-phenylketone / Aryl thioether / Benzoyl / Thiophenol ether / Imidazole-4-carbonyl group / Alkylarylthioether / Monocyclic benzene moiety / Benzenoid / Azole / Heteroaromatic compound/ Imidazole / Vinylogous amide / Urea / Sulfenyl compound / Organoheterocyclic compound / Thioether / Azacycle / Organic nitrogen compound / Organonitrogen compound / Organosulfur compound / Hydrocarbon derivative / Organic oxide / Organopnictogen compound / Aromatic heteromonocyclic compound|
|Molecular Framework||Aromatic heteromonocyclic compounds|
|External Descriptors||Not Available|
- Pharmacological action
- General Function:
- Metal ion binding
- Specific Function:
- Cyclic nucleotide phosphodiesterase with a dual-specificity for the second messengers cAMP and cGMP, which are key regulators of many important physiological processes.
- Gene Name:
- Uniprot ID:
- Uniprot Name:
- cGMP-inhibited 3',5'-cyclic phosphodiesterase A
- Molecular Weight:
- 124978.06 Da
- Boldt J, Suttner S: Combined use of ultra-short acting beta-blocker esmolol and intravenous phosphodiesterase 3 inhibitor enoximone. Expert Opin Pharmacother. 2007 Sep;8(13):2135-47. [PubMed:17714066 ]
- Sandroni C, Cavallaro F, Caricato A, Scapigliati A, Fenici P, Antonelli M: Enoximone in cardiac arrest caused by propranolol: two case reports. Acta Anaesthesiol Scand. 2006 Jul;50(6):759-61. [PubMed:16987374 ]